1995
DOI: 10.1002/ardp.19953280511
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Reduction of the Estrogenic Side Effects of the Mammary Tumor‐Inhibiting Drug [1,2‐Bis(2,6‐dichloro‐4‐hydroxyphenyl)‐ethylenediamine]dichloroplatinum(II) by Variation of Ring Substituents

Abstract: [1,2-Bis(4-methoxy/4-hydroxyphenyl)ethylenediamine]dichloroplatinum-(II) complexes with Cl-, CH3-, or OCH3-substituents in the ortho-positions of the aromatic rings (meso-1-PtCl2, D,L-1-PtCl2, meso-2-PtCl2, D,L-2-PtCl2, meso-3-PtCl2, meso-4-PtCl2, meso-5-PtCl2) were tested on the MDA-MB 231 breast cancer cell line, the lymphocytic leukemia P388, and the estrogen receptor-positive and -negative MXT mammary carcinoma of the mouse (MXT,ER(+)-MC, MXT,ER(-)-MC). The comparison of the effects of methoxy-substituted … Show more

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“…Several of these complexes strongly inhibit growth of hormone-dependent rat mammary tumours. (Anti)oestrogenic effects seem to prevail over a DNA damaging mode of action in those compounds which exhibit selectivity for hormone-sensitive tumours (Karl et al 1988;Schlemmer et al 1999;Gust et al 2000), whereas a lack of endocrine effects is mostly associated with either a loss of selectivity or even a total loss of activity (Gust and Schönenberger 1993;Gust et al 1995). Complexes containing 2-phenylindole ligands show a higher affinity for the oestrogen receptor and a marked selectivity for hormone-dependent tumours.…”
Section: Liposomal Platinum Drugsmentioning
confidence: 95%
“…Several of these complexes strongly inhibit growth of hormone-dependent rat mammary tumours. (Anti)oestrogenic effects seem to prevail over a DNA damaging mode of action in those compounds which exhibit selectivity for hormone-sensitive tumours (Karl et al 1988;Schlemmer et al 1999;Gust et al 2000), whereas a lack of endocrine effects is mostly associated with either a loss of selectivity or even a total loss of activity (Gust and Schönenberger 1993;Gust et al 1995). Complexes containing 2-phenylindole ligands show a higher affinity for the oestrogen receptor and a marked selectivity for hormone-dependent tumours.…”
Section: Liposomal Platinum Drugsmentioning
confidence: 95%